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BIX-01294 | BIX-01294 : Inhibitor of EHMT2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EHMT2
  • IC50:2.7 uM
Inhibitor
--

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - EHMT1 38 uM

Potency Assay Off-Target:
MS-based histone methyltransferase assay. No activity was detected up to 45 uM BIX-01294 against PRM ...
Selectivity Assessment Description:
Not available

Potency
Cellular
In Vitro

EHMT2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Orthogonal Probes def

A-366
UNC0642
UNC0638

Chemical Information

Molecular Formula C28H38N6O2
SMILEs COc1cc2nc(N3CCCN(C)CC3)nc(NC3CCN(Cc4ccccc4)CC3)c2cc1OC
InChI InChI=1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31)
Molecular weight 490.31 Da
AlogP 3.8654
HBond acceptors 8
HBond donors 1
Atoms 74

References

Publications

    Cross References

    canSARChEMBLBindingDBPDBe (Protein Data Bank Europe)

    Expert Reviews

    by SERP
    (on 4 Nov 2016 )
    Cellular Use Rating
    In Model Organisms
    Whilst there are many published references using this molecule in various cell-based studies, there is limited selectivity data disclosed for it beyond the closely associated family of proteins listed...
    by SERP
    (on 22 Dec 2016 )
    Cellular Use Rating
    In Model Organisms
    BIX-01294 should be used with caution. I have several specific concerns about this molecule: Selectivity over GLP is reportedly ~20x and >>20x for five related family members. Subsequent reports...
    by SERP
    (on 23 Jan 2017 )
    Cellular Use Rating
    Users should note selectivity experiments were performed against a limited panel of targets in the initial report. The lack of specificity data of BIX-01294 versus other targets (besides GLP, PRMT1,...
    The limited selectivity assessement of BIX-0194 within the HMT family and also outside the family restricts its usefulness. The compound is not very potent in vitro (low micromolar) and...
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